WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H317116
CAS#: 574013-66-4
Description: Fexaramine is an agonist of the farnesoid X receptor (FXR), which is a bile acid-activated nuclear receptor that controls bile-acid synthesis, conjugation and transport, as well as lipid metabolism through actions in the liver and intestine. Fexaramine has 100-fold greater affinity for FXR than natural compounds and described the genomic targets and binding site on FXR. When administered orally to mice, fexaramine produced selective actions through FXR receptors in the intestines.
Hodoodo Cat#: H317116
Name: Fexaramine
CAS#: 574013-66-4
Chemical Formula: C32H36N2O3
Exact Mass: 496.27
Molecular Weight: 498.650
Elemental Analysis: C, 77.39; H, 7.31; N, 5.64; O, 9.66
Synonym: Fexaramine
IUPAC/Chemical Name: methyl (E)-3-(3-(N-((4'-(dimethylamino)-[1,1'-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate
InChi Key: VLQTUNDJHLEFEQ-KGENOOAVSA-N
InChi Code: InChI=1S/C32H36N2O3/c1-33(2)29-19-17-27(18-20-29)26-15-12-25(13-16-26)23-34(32(36)28-9-5-4-6-10-28)30-11-7-8-24(22-30)14-21-31(35)37-3/h7-8,11-22,28H,4-6,9-10,23H2,1-3H3/b21-14+
SMILES Code: O=C(OC)/C=C/C1=CC=CC(N(C(C2CCCCC2)=O)CC3=CC=C(C4=CC=C(N(C)C)C=C4)C=C3)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. |
| In vitro activity: | BMMs differentiated into mature TRAP-positive (TRAP+) multinucleated osteoclasts (MNCs) during the culture period, while treatment with fexaramine inhibited osteoclast differentiation in a dose-dependent manner (Fig. 1A). Reference: J Bone Metab. 2017 Nov; 24(4): 207–215. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734945/ |
| In vivo activity: | This study finally evaluated the in vivo effect of fexaramine on osteoclast formation, using a LPS-challenged mouse model. In parallel with the effects in vitro, fexaramine notably reduced LPS-induced osteoclast formation (Fig. 5B). Collectively, this study conclude that fexaramine has an inhibitory effect on inflammation-induced osteoclastogenesis in vivo. Reference: J Bone Metab. 2017 Nov; 24(4): 207–215. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734945/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.6 | 73.30 | |
| DMF | 30.0 | 60.16 |
The following data is based on the product molecular weight 498.65 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Zheng T, Kim NY, Yim M. Fexaramine Inhibits Receptor Activator of Nuclear Factor-κB Ligand-induced Osteoclast Formation via Nuclear Factor of Activated T Cells Signaling Pathways. J Bone Metab. 2017 Nov;24(4):207-215. doi: 10.11005/jbm.2017.24.4.207. Epub 2017 Nov 30. PMID: 29259959; PMCID: PMC5734945. |
| In vitro protocol: | 1. Zheng T, Kim NY, Yim M. Fexaramine Inhibits Receptor Activator of Nuclear Factor-κB Ligand-induced Osteoclast Formation via Nuclear Factor of Activated T Cells Signaling Pathways. J Bone Metab. 2017 Nov;24(4):207-215. doi: 10.11005/jbm.2017.24.4.207. Epub 2017 Nov 30. PMID: 29259959; PMCID: PMC5734945. |
| In vivo protocol: | 1. Zheng T, Kim NY, Yim M. Fexaramine Inhibits Receptor Activator of Nuclear Factor-κB Ligand-induced Osteoclast Formation via Nuclear Factor of Activated T Cells Signaling Pathways. J Bone Metab. 2017 Nov;24(4):207-215. doi: 10.11005/jbm.2017.24.4.207. Epub 2017 Nov 30. PMID: 29259959; PMCID: PMC5734945. |
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